Two Double Bonds Between Ring Members Of The Five-membered Hetero Ring (e.g., Pyrrole, Etc.) Patents (Class 514/427)
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Patent number: 6013836Abstract: This invention relates to N'-substituted-N,N'-disubstitutedhydrazines of formula I ##STR1## wherein X and X' are independently O, S, or NR; A' and B' are independently substituted or unsubstituted aryl or aromatic heterocycle; wherein F is alkyl, alkenyl, or aralkyl; and wherein E is a tertiary carbon containing organic radical having a total of at least four carbon and halogen atoms but not more than six halogen atoms, or a non-tertiary carbon containing non-haloalkyl organic or organometallic radical having at least five atoms other than hydrogen, oxygen and halogen which are useful as insecticides, compositions containing those compounds, methods of producing the compounds, and methods of their use. More particularly, the invention relates to insect growth regulating compounds and compositions, and methods of using such compounds and compositions. Compounds of the present invention are particularly suitable for controlling plant-destructive insects in crops of cultivated plants, ornamentals and forestry.Type: GrantFiled: May 22, 1995Date of Patent: January 11, 2000Assignee: Rohm and Haas CompanyInventors: Adam Chi-Tung Hsu, Harold Ernest Aller, Dat Phat Le, Donald Wesley Hamp, Barry Weinstein, Raymond August Murphy
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Patent number: 6008243Abstract: The present invention is directed to compound of the formula I: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, X, Y, and ##STR2## are as defined herein. These compounds are useful for inhibiting the activity of a metalloproteinase by contacting the metalloproteinase with an effective amount of the inventive compounds.Type: GrantFiled: March 25, 1997Date of Patent: December 28, 1999Assignees: Agouron Pharmaceuticals, Inc., Syntex (U.S.A.), Inc.Inventors: Steven L. Bender, Arlindo L. Castelhano, Wesley K. M. Chong, Melwyn A. Abreo, Jian Jeffrey Chen, Judith G. Deal
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Patent number: 6008219Abstract: This invention relates to compounds of formula (I) ##STR1## which are useful as modulators of D.sub.3 receptors, in particular as antipsychotic agents.Type: GrantFiled: October 29, 1997Date of Patent: December 28, 1999Assignee: SmithKline Beech p.l.c.Inventors: Geoffrey Stemp, Christopher Norbert Johnson
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Patent number: 5998459Abstract: The invention relates to a pharmaceutical composition comprising a pyrrole derivative of the following formula [1] or a pharmaceutically acceptable salt thereof, or a solvate of either of them, as an active ingredient. ##STR1## (wherein R.sup.1 represents hydrogen or alkoxycar91 bonylamino, R.sup.2 represents alkyl, aryl which may be substituted, aromatic heterocyclyl which may be substituted, unsubstituted amino, monoalkylamino, dialkylamino, or cyclic amino which may be substituted; R.sup.3 represents cyano or carbamoyl; R.sup.4 represents hydrogen or alkyl; E represents alkylene; q is equal to 0 or 1, A represents methyl, aryl which may be substituted, or aromatic heterocyclyl which may be substituted). The pharmaceutical composition of the invention is effective for the treatment of pollakiuria or urinary incontinence.Type: GrantFiled: December 8, 1997Date of Patent: December 7, 1999Inventors: Masami Tsuda, Mitsushi Tanaka, Ayatsugu Nakamura
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Patent number: 5994389Abstract: The invention relates to novel substituted N-aryl- and N-alkylsulfonylaminals of the formula (I) in whichA represents specific N-heterocycles specified in the description and R.sup.1, R.sup.2 and R.sup.3 have the meaning given in the description, to a process for their preparation and to their use as agents for combating pests.Type: GrantFiled: August 21, 1997Date of Patent: November 30, 1999Assignee: Bayer AktiengesellschaftInventors: Bernd Baasner, Hermann Hagemann, Markus Heil, Folker Lieb, Hermann Uhr, Christoph Erdelen
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Patent number: 5965602Abstract: The present invention provides a pesticidal composition which comprises 4-bromo-2-(4-chlorophenyl)-1-ethoxymethyl-5-trifluromethylpyrrole-3-carbon itrile and at least one pyrethroidal compound as active ingredients, and an inert carrier, and an insecticidal/acaricidal method applying 4-bromo-2-(4-chlorophenyl)-1-ethoxymethyl-5-trifluoromethylpyrrole-3-carbo nitrile and at least one pyrethroidal compound to noxious insects, acarina, or the locus where noxious insects or acarina inhabit.Type: GrantFiled: October 30, 1996Date of Patent: October 12, 1999Assignee: Sumitomo Chemical Company Ltd.Inventors: Yoji Takada, Izumi Fujimoto
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Patent number: 5948779Abstract: Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes are useful for inducing or promoting apotosis and for arresting uncontrolled neoplastic cell proliferation, and are specifically useful in the arresting and treatment of neoplasias, including precancerous and cancerous lesions.Type: GrantFiled: December 12, 1997Date of Patent: September 7, 1999Assignee: Cell Pathways, Inc.Inventors: Gerhard J. Sperl, Paul Gross, Klaus Brendel, Gary A. Piazza, Rifat Pamukcu
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Patent number: 5945441Abstract: This invention relates to methods of treating hair loss, through hair revitalization and germination, by administering non-immunosuppresive pyrrolidine carboxylate compounds.Type: GrantFiled: June 4, 1997Date of Patent: August 31, 1999Assignee: Gpi Nil Holdings, Inc.Inventors: Joseph P. Steiner, Gregory S. Hamilton
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Patent number: 5942548Abstract: Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of cardiovascular disorders. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.Type: GrantFiled: March 24, 1998Date of Patent: August 24, 1999Assignee: G.D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5942538Abstract: The present invention relates to benzamidoxime derivatives represented by the formula ?I!; ##STR1## wherein R.sup.1 is unsubstituted or substituted C.sub.1 -C.sub.4 alkyl, unsubstituted or substituted C.sub.2 -C.sub.4 alkenyl or unsubstituted or substituted C.sub.2 -C.sub.4 alkynyl, R.sup.2 is phenyl optionally having substituents or heterocycle optionally having substituents X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are each independently hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.1 -C.sub.4 alkylthio or the like, and r.sub.1 and r.sub.2 are each independently hydrogen, C.sub.1 -C.sub.4 alkyl or the like, having excellent fungicidal activity and being useful as a fungicide for agricultural and horticultural use, and methods for preparation thereof.Type: GrantFiled: June 26, 1998Date of Patent: August 24, 1999Assignee: Nippon Soda Co., Ltd.Inventors: Isamu Kasahara, Hirohito Ooka, Shinsuke Sano, Hiroyasu Hosokawa, Homare Yamanaka
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Patent number: 5935990Abstract: A class of pyrrolyl derivatives is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as described in the specification.Type: GrantFiled: December 9, 1997Date of Patent: August 10, 1999Assignee: G.D. Searle & Co.Inventors: Ish K. Khanna, Richard M. Weier, Yi Yu
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Patent number: 5932520Abstract: There is provided a method for controlling or combatting the attachment of a fouling organism to an underwater surface which comprises contacting said organism with an antifouling-effective amount of a 2-arylpyrrole compound. A method for protecting aquatic structures against fouling by a marine or freshwater fouling organism and antifoulant compositions therefor are also provided.Type: GrantFiled: May 23, 1995Date of Patent: August 3, 1999Assignee: American Cyanamid CompanyInventors: Mark Arthur Josepha Van der Flass, Lantz Stephen Crawley
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Patent number: 5929114Abstract: Arylthiol and dithiobisarylamide antibacterial and antiviral agents have the general formula ##STR1## where A is monocyclic or bicyclic aryl which can contain up to 3 heteroatoms selected from O, S, and N,R.sup.1 and R.sup.2 are substituent groups, X is ##STR2## or SO.sub.2 NR.sup.4 Z, Y is H or SZ when n is 1, a single bond when n is 2; R.sup.4 and Z can be hydrogen or alkyl.Type: GrantFiled: May 15, 1997Date of Patent: July 27, 1999Assignee: Warner-Lambert CompanyInventors: John Michael Domagala, Edward Faith Elslager, Rocco Dean Gogliotti
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Patent number: 5925654Abstract: The present invention provides compounds having the structure: ##STR1## and pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.Type: GrantFiled: March 12, 1997Date of Patent: July 20, 1999Assignee: G.D. Searle & Co.Inventors: Barbara Baosheng Chen, Helen Chen, Mark Andrew Russell, Julie Marion Miyashiro, James Malecha, Thomas Dale Penning
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Patent number: 5925631Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: August 3, 1998Date of Patent: July 20, 1999Assignee: Merck & Co., Inc.Inventors: Cameron Black, Greg Hughes, Erich Grimm, Serge Leger, Petpiboon Prasit, Zhaoyin Wang
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Patent number: 5922887Abstract: A compound, or solvate or salt thereof, of formula (I) ##STR1## in which, R.sub.1 and R.sub.2, are, independently hydrogen, linear or branched C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkenyl, or C.sub.3-6 alkenyl, or together form a C.sub.3-7 alkyl;R.sub.3 and R.sub.4 are, independently, hydrogen, linear or branched C.sub.1-6 alkyl, or R.sub.4 is oxygen forming with the carbon atom to which is attached a C.dbd.O group;R.sub.5 is hydrogen, hydroxy, or C.sub.1-3 alkoxy;R.sub.6 is halogen, NH.sub.2 or a para or meta --COR-8 group, in which R.sub.8 is C.sub.1-8 -alkyl, C.sub.1-8 -alkoxy or NR.sub.9 R.sub.10, wherein R.sub.9 and R.sub.10, are, independently, hydrogen, straight or branched C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl or phenyl; or R.sub.6 is a para or meta group ##STR2## in which R.sub.11 and R .sub.12 are, independently, hydrogen or straight or branched C .sub.1-6 and,R.sub.7 is hydrogen, or straight or branched C.sub.1-8 alkyl; is provided.Type: GrantFiled: November 18, 1997Date of Patent: July 13, 1999Assignee: SmithKline Beecham SpAInventors: Giulio Dondio, Silvano Ronzoni
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Patent number: 5919786Abstract: The present invention relates to a compound of the formula (I): ##STR1## wherein Ar.sup.1, Ar.sup.2, Ar.sup.3 and Ar.sup.4 represent an aryl group or a heteroaromatic ring group; A represents a hydrocarbon group which may be substituted; X and Y represent an oxygen atom, a sulfur atom, a carbonyl group or a group of the formula --CHR.sup.a -- (wherein R.sup.a is a hydrogen atom or a lower alkyl group) or --NR.sup.b -- (wherein R.sup.b is a hydrogen atom or a lower alkyl group), or X and Y together represent a vinylene group or an ethynylene group; R.sup.1, R.sup.2, R.sup.3, R.sup.8 and R.sup.9 represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group; R.sup.4 and R.sup.Type: GrantFiled: March 25, 1998Date of Patent: July 6, 1999Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshikazu Iwasawa, Tetsuya Aoyama, Kumiko Kawakami, Sachie Arai, Toshihiko Satoh, Yoshiaki Monden
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Patent number: 5919774Abstract: A class of novel pyrroles is disclosed together with the use of such compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.Type: GrantFiled: December 5, 1997Date of Patent: July 6, 1999Assignee: Eli Lilly and CompanyInventors: Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim
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Patent number: 5908858Abstract: Compounds of formula (I) and (II): ##STR1## ?wherein R is hydrogen, halogen or alkyl; R.sup.1 is alkyl, amino or substituted amino; R.sup.2 is optionally substituted phenyl; R.sup.3 is hydrogen, halogen or optionally substituted alkyl; R.sup.4 is hydrogen, optionally substituted alkyl, cycloalkyl, aryl, or aralkyl! have valuable analgesic, anti-inflammatory, anti-pyretic and anti-allergic activities and have the ability to inhibit the production of leukotrienes and to inhibit bone resorption. They are relatively free from the side effects which generally result from the administration of compounds having these kinds of activities.Type: GrantFiled: March 26, 1997Date of Patent: June 1, 1999Assignee: Sankyo Company, LimitedInventors: Tomio Kimura, Yasuo Noguchi, Akira Nakao, Keisuke Suzuki, Shigeru Ushiyama, Akihiro Kawara, Masaaki Miyamoto
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Patent number: 5891901Abstract: Compounds of the formula ##STR1## wherein R is alkyl, alkylthio or hydroxy, as well as, pharmaceutically acceptable salts of compounds of formula I are antiproliferative agents useful in the treatment of cancer.Type: GrantFiled: July 24, 1997Date of Patent: April 6, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Urvashi Hooda Dhingra, Donna Mary Huryn, Dennis Dalton Keith, Giuseppe Federico Weber
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Patent number: 5889031Abstract: Certain N-acyl 2-aryl cyclopropylmethylamine derivatives are useful as melatonergic agents.Type: GrantFiled: February 9, 1998Date of Patent: March 30, 1999Assignee: Bristol-Myers Squibb CompnayInventors: Daniel J. Keavy, Michael F. Parker, Ronald J. Mattson, Graham Johnson
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Patent number: 5883106Abstract: Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having the following formula I: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Ar.sup.1 is a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, which is bonded to X.sup.1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, and C.sub.1-4 alkyl; X.sup.1 is a direct bond or C.sub.1-4 alkylene; Ar.sup.2 is phenylene optionally substituted with halo, hydroxy, cyano, and amino X.sup.2 is --A--X-- or --X--A-- wherein A is a direct bond or C.sub.1-4 alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar.sup.3 is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino and C.sub.1-4 alkyl; R.sup.1 and R.sup.2 are each C.sub.Type: GrantFiled: February 6, 1998Date of Patent: March 16, 1999Assignee: Pfizer Inc.Inventors: Rodney W. Stevens, Takashi Mano, Kazunari Nakao, Yoshiyuki Okumura
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Patent number: 5877196Abstract: The present invention relates to substituted .omega.-?phenoxy, phenylthio, phenylsulfinyl, phenylsulfonyl! ?alkyl, alkenyl or alkynyl!amine carboxamides, sulfonamides and phosphonylamides which are useful as antiarrhythmic agents.Type: GrantFiled: February 14, 1997Date of Patent: March 2, 1999Assignee: American Cyanamid CompanyInventors: Andrew Stephen Tomcufcik, Joseph William Hinson
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Patent number: 5872117Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.Type: GrantFiled: November 4, 1997Date of Patent: February 16, 1999Assignee: Toyama Chemical Co., Ltd.Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita
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Patent number: 5872129Type: GrantFiled: July 31, 1997Date of Patent: February 16, 1999Assignee: Auckland UniServices LimitedInventors: William Alexander Denny, William Robert Wilson, Moana Tercel
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Patent number: 5869521Abstract: Anti-pruritic pharmaceutical formulations containing kappa agonist compounds and methods of prevention or treatment of pruritus in a mammal with the anti-pruritic formulations.Type: GrantFiled: April 22, 1998Date of Patent: February 9, 1999Assignee: Adolor CorporationInventors: John J. Farrar, An-Chih Chang, Virendra Kumar, Wei Yuan Zhang, Alan Cowan
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Patent number: 5869067Abstract: The present invention relates to new aromatic compounds, to their preparation and to their use in human and veterinary medicine and in cosmetic compositions.Type: GrantFiled: September 26, 1994Date of Patent: February 9, 1999Assignee: Centre International De Recherches Dermatologiques Galderma (CIRD Galderma)Inventors: Jean-Phillippe Rocher, Jean-Michel Bernardon
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Patent number: 5859048Abstract: In pharmaceutics for mucosal administration containing pharmacologically active peptides or proteins and tolmetin or salts thereof exhibited very excellent effect as mucosal absorption enhancers.Furthermore, when the pharmaceutics for mucosal administration are for rectal administration, the suppository in which at least either the active ingredient, peptide or protein, or the mucosal absorption enhancer is converted to a complex with a high molecular compound dissolving in water at pH 5 or higher and together uniformly dispersed in a fatty suppository base exhibited markedly improved rectal absorbability compared with that of conventional pharmaceutics for rectal administration and at the same time increased stability of the peptide or protein which is the active ingredient.Type: GrantFiled: June 25, 1997Date of Patent: January 12, 1999Assignee: Teikoku Hormone MFG. Co., Ltd.Inventors: Masami Oohashi, Noriaki Uchida, Junichi Sakata, Masaru Sunamoto
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Patent number: 5849775Abstract: Benzoylguaridines of the formula I ##STR1## are described in which: R(1), R(2), R(3), R(4), R(5) are as defined in the specification, and pharmaceutically tolerated salts thereof.Type: GrantFiled: June 30, 1997Date of Patent: December 15, 1998Assignee: Hoechst AktiengesellschaftInventors: Jan-Robert Schwark, Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Wolfgang Scholz, Udo Albus
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Patent number: 5843983Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 represents a saturated heterocyclic group attached to the bond or group represented by A through a ring carbon atom; R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3a, R.sup.3b, R.sup.3c and R.sup.3d are hydrogen or various other groups or atoms; and A represents a single bond or an alkylene group having from 1 to 6 carbon atoms are serotonin 2 receptor antagonists and have the ability to inhibit the activity of squalene synthase. They can not only prevent and inhibit the development and progression of arteriosclerosis but can also inhibit thrombosis in arteriosclerotic lesions and can improve hemodynamics.Type: GrantFiled: February 10, 1997Date of Patent: December 1, 1998Assignee: Sankyo Company, LimitedInventors: Koichi Fujimoto, Naoki Tanaka, Fumitoshi Asai, Taketoshi Ogawa, Teiichiro Koga, Tatsuo Tanimoto, Yoshio Tsujita, Hiroyuki Koike
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Patent number: 5837703Abstract: Therapeutic compounds have the formula:(X)j-(core moiety),j being an integer from one to three, the core moiety comprising a core moiety, the core moiety being a heterocycle having one ring or two-fused rings, each ring having five or six ring atoms, A being a carbon atom of the core moiety and attached to a terminal carbon atom of (CH.sub.2).sub.m, and X has a structure and X being a racemic mixture, R or S enantiomer, solvate, hydrate, or salt of: ##STR1## *C is a chiral carbon atom, n is an integer from one to four (preferably from one to three), one or more carbon atoms of (CH.sub.2).sub.n may be substituted by a keto or hydroxy group, and m is an integer from one to fourteen. Independently, R.sub.1 and R.sub.2 may be a hydrogen, a straight or branched chain alkyl or alkenyl of up to twelve carbon atoms in length, or --(CH.sub.2).sub.w R.sub.5, w being an integer from two to fourteen and R.sub.5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R.sub.Type: GrantFiled: November 12, 1993Date of Patent: November 17, 1998Assignee: Cell Therapeutics, Inc.Inventors: Anil M. Kumar, John Michnick, Gail E. Underiner, J. Peter Klein, Glenn C. Rice
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Patent number: 5824691Abstract: Guanidine derivatives of the formula: ##STR1## wherein Y is C--R.sup.1(in which R.sup.1 is hydrogen, lower alkyl, hydroxy, protected hydroxy, etc.,)R.sup.2 is pyrrolyl, tetrazolyl, pyrazolyl, etc.,R.sup.3 is hydrogen, lower alkoxy, hydroxy, protected hydroxy, etc.,Z is C--R.sup.4(in which R.sup.4 is hydrogen, carboxy, protected carboxy, nitro, halogen, hydroxy(lower)alkyl, etc.,), andW is R.sup.12(in which R.sup.12 is hydrogen, lower alkoxy, nitro, hydroxy or protected hydroxy)and pharmaceutically acceptable salts thereof which are useful as a medicament which are useful in inhibiting Na.sup.+ /H.sup.+ exchange in cells and in the prevention of cardiovascular diseases, cerebrovascular diseases, renal diseases, arteriosclerosis and shock.Type: GrantFiled: November 9, 1995Date of Patent: October 20, 1998Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Atsushi Kuno, Yoshikazu Inoue, Hisashi Takasugi, Hiroaki Mizuno, Kumi Yamasaki
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Patent number: 5811410Abstract: A method of administering a medicinal agent and an effective amount of a form of hyaluronic acid for decreasing side effects associated with using the agent alone in treating a disease or condition in mammals is disclosed. The agent may be a non-steroidal anti-inflammatory drug (NSAID). The amount of hyaluronic acid is sufficient enough to provide a dosage greater than 200 mg/70 kg person. The molecular weight of the form of hyaluronic acid may be less than 750,000 daltons.Type: GrantFiled: June 5, 1995Date of Patent: September 22, 1998Assignee: Hyal Pharmaceutical CorporationInventors: Rudolf Edgar Falk, Samuel S. Asculai
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Patent number: 5792786Abstract: The present invention provides therapeutic conjugates which comprise a therapeutic compound bound to one to three acyl groups derived from fatty acids. The therapeutic compounds are preferably non.about.steroidal anti.about.inflammatory agents which include a carboxylic acid group. The compounds involve the use of tromethamine or ethanolamine derivative to link the acyl groups derived from fatty acids to the therapeutic compounds.Type: GrantFiled: April 12, 1996Date of Patent: August 11, 1998Assignee: Commonwealth Scientific and Industrial Research OrganisationInventors: Robert George Whittaker, Veronika Judith Bender, Wayne Gerrard Reilly
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Patent number: 5792778Abstract: The present invention addresses 2-substituted aryl pyrroles, as well as compositions containing such compounds and methods of treatment. Cytokine mediated diseases refers to diseases or conditions in which excessive or unregulated production or activity of one or more cytokines occurs. Interleukin-1 (IL-1), Interleukin-6 (IL-6), Interleukin-8 (IL-8) and Tumor Necrosis Factor (TNF) are cytokines which are involved.Type: GrantFiled: August 8, 1996Date of Patent: August 11, 1998Assignee: Merck & Co., Inc.Inventors: Stephen E. de Laszlo, Nigel J. Liverton, Gerald S. Ponticello, Harold G. Selnick, Nathan B. Mantlo
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Patent number: 5767151Abstract: The present invention relates to novel 3,3-(disubstituted)-cyclohexan-1-ylidene acetate dimers of Formula (I): ##STR1## and related compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammateory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).Type: GrantFiled: June 23, 1997Date of Patent: June 16, 1998Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski
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Patent number: 5756426Abstract: Described herein are compounds of the formula I ##STR1## and the isomers thereof, in which either a) X is an N atom andY is OR.sub.11 or N(R.sub.12)R.sub.13, orb) X is CH andY is OR.sub.11,and in which furthermore:R.sub.11 is C.sub.1 -C.sub.4 alkyl;R.sub.12 and R.sub.13, independently, are hydrogen or C.sub.1 -C.sub.4 alkyl;A is an O atom or the group NR.sub.4 ; and whereinR.sub.1, R.sub.2 and R.sub.3 are as defined herein, are pesticidal active ingredients. They can be used for pest control, in particular as microbicides, insecticides and acaricides in agriculture, horticulture and in the hygiene sector.Type: GrantFiled: September 11, 1995Date of Patent: May 26, 1998Assignee: Novartis CorporationInventors: Hugo Ziegler, Stephan Trah, Saleem Farooq, Rene Zurfluh
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Patent number: 5753680Abstract: Heterocyclyl-benzoylguanidines of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and Het have the meanings given herein, and physiologically unobjectionable salts thereof, display antiarrhythmic properties and act as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.Type: GrantFiled: August 30, 1995Date of Patent: May 19, 1998Assignee: Merck Patent Gesellschaft MIT Beschrankter HaftungInventors: Rolf Gericke, Dieter Dorsch, Manfred Baumgarth, Klaus-Otto Minck, Norbert Beier
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Patent number: 5747523Abstract: The invention relates to substituted ethyl .alpha.,.alpha.-diarylmethyl ether derivatives and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same, and methods of treating cocaine addiction and overdose, and diseases and conditions characterized by abnormal dopaminergic neurotransmission, using the same.Type: GrantFiled: January 24, 1996Date of Patent: May 5, 1998Assignee: Guilford Pharmaceuticals Inc.Inventor: Paul F. Jackson
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Patent number: 5731335Abstract: This invention provides heterocyclic compounds of formula (I) that are potentially useful in the treatment of neuropsychiatric disorders associated with progressive processes leading to neuronal necrosis and dysfunction. In particular, the novel compounds which do not bind to muscarinic receptors are inhibitors of delayed neuronal death as shown in the gerbil bilateral occlusion model of ischemia.Type: GrantFiled: March 6, 1995Date of Patent: March 24, 1998Assignee: Astra AktiebolagInventors: Robin Bernad Boar, Alan John Cross, Duncan Alastair Gray, Richard Alfred Green
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Patent number: 5723499Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(i): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: December 15, 1994Date of Patent: March 3, 1998Assignee: C.I.R.D. GaldermaInventors: Bruno Charpentier, Jean-Michel Bernardon
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Patent number: 5723470Abstract: Novel 3,4,4-trifluorobutenoic acid derivatives of the formula ##STR1## wherein Q is --(C.dbd.W)--R.sub.2 wherein W is O or S, and R.sub.2 is an aliphatic or aromatic group when W.dbd.O; --OR.sub.50 ; --SR.sub.50 ; or --NR.sub.50 R.sub.60 wherein R.sub.60 is hydrogen or R.sub.50 ; NR.sub.7 R.sub.8 ; a heterocyclic group; phenyl substituted by alkyl; or any agronomically acceptable salt thereof having usefulness as nematocides, insecticides and acaricides.Type: GrantFiled: February 12, 1996Date of Patent: March 3, 1998Assignee: Monsanto CompanyInventors: Dennis Paul Phillion, Peter Gerrard Ruminski, Gopichand Yalamanchili
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Patent number: 5719169Abstract: The invention relates to benzoylguanidines of the formula I: ##STR1## to pharmaceutically acceptable salts of these compounds and to a process for preparing compounds of the formula I, which comprise reacting a compound of the formula II ##STR2## with guanidine. The compounds of the invention are suitable as antiarrhythmic pharmaceuticals having a cardioprotective component for the prophylaxis and treatment of infarction and for the treatment of angina pectoris.Type: GrantFiled: July 3, 1996Date of Patent: February 17, 1998Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
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Patent number: 5710140Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: August 16, 1996Date of Patent: January 20, 1998Assignee: Merck Frosst Canada, Inc.Inventors: Yves Ducharme, Jacques Yves Gauthier, Petpiboon Prasit, Yves Leblanc, Zhaoyin Wang, Serge Leger, Michel Therien
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Patent number: 5703073Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.Type: GrantFiled: October 13, 1995Date of Patent: December 30, 1997Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Patent number: 5696150Abstract: A novel fungicidal composition comprising a fungicidally effective amount of a combination consisting of(i) N-?1-(4-chloro-phenyl)-ethyl!-2,2-dichloro-1-ethyl-3-methyl-cyclopropaneca rboxamide of the formula ##STR1## and (ii) (A) a triazole derivative of the formula ##STR2## in which X represents chlorine or phenyl, and/or (B) a pyrrole derivative of the formula ##STR3## in which R represents ##STR4## and/or (C) the imidazole derivative of the formula ##STR5## The novel composition shows a synergistic activity.Type: GrantFiled: September 13, 1996Date of Patent: December 9, 1997Assignee: Bayer AktiengesellschaftInventors: Gerd Hanssler, Stefan Dutzmann, Matthias Wunsch
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Patent number: 5691337Abstract: Oxy-phenyl-(phenyl)glycinolamides with heterocyclic substituents are prepared by reaction of the corresponding oxyphenylcarboxylic acids with heterocyclic substituents with phenylglycinol. The new substances are suitable as active compounds in medicaments, in particular in agents having an antiatherosclerotic action.Type: GrantFiled: January 13, 1997Date of Patent: November 25, 1997Assignee: Bayer AktiengesellschaftInventors: Ulrich Muller, Richard Connell, Siegfried Goldmann, Klaus-Helmut Mohrs, Siegfried Raddatz, Michael Matzke, Rudi Grutzmann, Martin Beuck, Stefan Wohlfeil, Hilmar Bischoff, Dirk Denzer
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Patent number: 5686476Abstract: This invention encompasses methods for the inhibition of Alzheimer's Disease comprising administering to a human in need thereof an effective amount of a compound of Formula I ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethylenemino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.The present invention also provides methods of increasing TGF-.beta. expression in the brain, comprising administering to a human in need thereof an effective amount of a compound of formula 1.The present invention also provides methods of inhibiting the .beta.-amyloid peptide mediated neurotoxicity or inflammatory response associated with Alzheimer's Disease (AD) comprising administering to a human in need thereof an effective amount of a compound of formula 1.Type: GrantFiled: March 15, 1995Date of Patent: November 11, 1997Assignee: Eli Lilly and CompanyInventor: Patrick C. May
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Patent number: 5686467Abstract: A method of inhibiting imperfect tissue repair or a physiological condition due at least in part thereto comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.Type: GrantFiled: March 15, 1995Date of Patent: November 11, 1997Assignee: Eli Lilly and CompanyInventors: Thomas F. Bumol, George J. Cullinan
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Patent number: RE36419Abstract: The present invention provides novel methods for prevention or treatment of primary and recurring squamous cell carcinoma of the oral cavity or oropharynx comprising topical administration, to the oral cavity or oropharynx, of an effective amount of an NSAID, especially a composition administering from about 0.001% to about 0.2% ketorolac to the oral cavity, alone or as an adjunct to surgery and/or radiation therapy.Type: GrantFiled: March 27, 1998Date of Patent: November 30, 1999Assignee: The Procter & Gamble CompanyInventor: Paul Francis Cavanaugh, Jr.